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20

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T15622	JNJ-54175446 JNJ-5446	P2X Receptor	Membrane transporter/Ion channel; Neuroscience
	JNJ-54175446 (JNJ-5446) 是一种具有中枢神经系统渗透性和选择性的 P2X7 受体拮抗剂，可减弱小胶质细胞 IL-1β/IL-18 的释放，可用于研究抑郁症。
T36347	Ac-YVAD-CMK Caspase-1 Inhibitor II,Ac-Tyr-Val-Ala-Asp-chloromethylketone,Ac-Tyr-Val-Ala-Asp-CMK	IL Receptor; Caspase; Immunology/Inflammation related; Pyroptosis	Apoptosis; Immunology/Inflammation; Proteases/Proteasome
	Ac-YVAD-CMK (Ac-Tyr-Val-Ala-Asp-CMK) 是一种选择性的、不可逆的Caspase-1抑制剂，并能抑制焦亡作用、IL-1β和IL-18。Ac-YVAD-CMK 显示出神经保护和抗炎的能力。
T6090	Belnacasan VX-765	Caspase	Apoptosis; Proteases/Proteasome
	Belnacasan (VX-765) 是一种具有口服活性的 IL 转换酶/caspase-1 抑制剂，是 VRT-043198 的口服生物活性前药，作用于外周血单核细胞，可抑制 LPS 诱导的 IL-1β 和 IL-18 释放。
TP2008L	Lyn peptide inhibitor acetate Lyn peptide inhibitor acetate(222018-18-0 free base)	IL Receptor	Immunology/Inflammation
	Lyn peptide inhibitor acetate(222018-18-0 free base) 是一种有效的细胞渗透性 Lyn 偶联 IL-5 受体信号通路抑制剂，同时保持其他信号完整。它阻断 Lyn 活化并抑制 Lyn 酪氨酸激酶与 IL-3/GM-CSF/IL-5 受体的 βc 亚基的结合。它可用于哮喘、过敏和其他嗜酸性粒细胞疾病的研究。
T16570	Pralnacasan VX-740,HMR 3480	Others	Others
	Pralnacasan inhibits proinflammatory cytokines IL-18, IL-1β , and IFN-γ. Pralnacasan is an effective, non-peptide, and orally active interleukin-1β converting enzyme inhibitor (Ki: 1.4 nM). Pralnacasan has the potential for osteoarthritis and rheumatoid a
T70905	TLR9-IN-18
	TLR9-IN-18 is a potent and selective TLR9 antagonist. TLR9-IN-18 suppresses the production of the proinflammatory cytokine IL-6 in a CpG-induced mouse model.
T81668	NLRP3 agonist 1	NOD-like Receptor (NLR)	Immunology/Inflammation
	NLRP3 agonist1 (compound 23)为高效口服活性NLRP3激动剂。该化合物能够激活Caspase-1酶，进而将pro-IL-1β与pro-IL-18等促炎细胞因子裂解为成熟型态。
T76938	Camoteskimab
	Camoteskimab (AVTX-007)为全人源、高亲和力抗IL-18单克隆抗体，展现于自身炎症性疾病研究潜力，包括成人斯蒂尔病(AOSD)。
T10447	BAA473	Others	Others
	BAA473 是胆汁酸类似物，是一种强效的吡喃类炎症小体激活剂。BAA473可通过激活髓样和肠上皮细胞中的炎症小体来诱导白细胞介素（ IL-18 ）的分泌。
T78822	JT002	NOD-like Receptor (NLR)	Immunology/Inflammation
	JT002为口服活性的NLRP3炎性体抑制剂，能够抑制NLRP3依赖性促炎细胞因子（如IL-1β、IL-1α、IL-18）的生成以及细胞焦亡（pyroptosis），阻断NLRP3炎性体复合物的形成。此外，JT002可有效减少小鼠气道高反应性，并降低气道中中性粒细胞的聚集。
T61621	IMMH001
	IMMH001, also known as SYL930, is an orally active compound that exhibits potent selectivity as an agonist for the S1P1 receptor, which is the sphingosine-1-phosphate receptor 1. This compound effectively reduces the levels of various chemokines and proinflammatory cytokines, such as IL-1β, IL-5, IL-18, IP10, CCL3, and CCL5. IMMH001 finds utility in research focused on rheumatoid arthritis (RA) [1] [2].
T68225	Fc 11a-2
	Fc 11a-2 是一种苯并咪唑化合物，一种具有口服活性且有效的NLRP3炎症小体 (NLRP3inflammasome) 抑制剂。Fc 11a-2 通过抑制caspase-1的激活进而抑制 IL-1b/IL-18 的激活来抑制NLRP3炎性体的形成。Fc 11a-2 可防止Dextran sulfate sodium(DSS) 诱导的小鼠实验性结肠炎。
T81579	P2X7 receptor antagonist-4
	P2X7 receptor antagonist-4（Compound 14a）是一种选择性P2X7R拮抗剂，其对人类和小鼠P2X7R的IC50值分别为64.7 nM和10.1 nM。该化合物能有效抑制NLRP3炎性体的激活，并在脓毒症模型小鼠中减少肾损伤，降低caspase-1、gasdermin D、IL-1β和IL-18的表达。
T37458	C18 Phytoceramide (t18:0/18:0)
	C18 Phytoceramide (t18:0/18:0) (Cer(t18:0/18:0)) is a bioactive sphingolipid found in S. cerevisiae, wheat grains, and the stratum corneum layer of mammalian epidermis. Cer(t18:0/18:0) is composed of a phytosphingosine backbone amine-linked to a C18 fatty acid chain. Cer(t18:0/18:0) has a role in regulation of apoptosis, cell differentiation, proliferation of smooth muscle cells, and inhibition of the mitochondrial respiratory chain. It also inhibits expression of the allergic cytokines IL-4, TN...
T74908	ODN 2336
	ODN 2336 是 A 类 CpG ODN（寡脱氧核苷酸），是一种有效的 TLR9激动剂。ODN 2336 诱导 IFN-α 的产生。ODN 2336 上调 IP-10 mRNA 和 IL-18mRNA 的表达。ODN 2336 可用作疫苗的佐剂。
T36320	C6 L-threo Ceramide (d18:1/6:0) C6 L-threo Ceramide (d18:1/6:0)
	C6 L-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides., C6 L-threo Ceramide is cytotoxic to U937 cells in vitro (IC50 = 18 μM). It is metabolically inactive and, unlike C6 L-erythro ceramide , C6 L-threo ceramide cannot be converted to C6 glucosylceramide by ceramide glucosyltransferase. C6 L-threo Ceramide enhances IL-4 production induced by phorbol 12-myristate 13-acetate in EL4 T cells when used at a concentration of 10 μM.
T37565	C6 D-threo Ceramide (d18:1/6:0) C6 D-threo Ceramide (d18:1/6:0)
	C6 D-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides., C6 D-threo Ceramide is cytotoxic to U937 cells in vitro (IC50 = 18 μM). It is metabolically inactive and, unlike C6 L-erythro ceramide , C6 D-threo ceramide cannot be converted to C6 glucosylceramide by ceramide glucosyltransferase. C6 D-threo Ceramide promotes survival of isolated rat spinal neurons when used at concentrations up to 2.5 μM but induces cell death at concentrations greater...
T69815	SB-284851-BT
	SB-284851-BT 是一种 BRD4/p38α/BRDT 抑制剂。SB-284851-BT 抑制BRD4-BD1(IC50=1.7 µM)、p38α(Kd=0.47 nM)、BRDT(1) (IC50=18 µM) 和BRD4(1) (IC50=3.7 µM)。SB-284851-BT 通过抑制p38α以减少IL-8的产生，抑制BRD4以下调癌症的c-Myc 和NF-κB 基因通路。SB-284851-BT 能与溴结构域和超末端结构域 (BET) 结合。
T36629	Givinostat
	Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat (ITF2357) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduced IL-1β secretion more than 70%. Givinostat (ITF-2357) suppresses the production of IL-6 in PBMCs stimulated with TLR agonists as well as the combination of IL-12 plus IL-18. IL-6 secretion decreases to 50% at 50 nM Givinostat, but at 1...
T37614	LDN-0088050
	LDN 0088050 is selectivity adipocyte fatty acid binding protein (AFABP, FABP4) inhibitor with Ki values of 0.29 and 1.3 μM for FABP4 and FABP3, respectively. LDN 0088050 binds to FABP4 with a Kd of 2.05 μM[1]. Ki: 0.29 μM (FABP4), 1.3 μM (FABP3)[1]Kd: 2.05 μM (FABP4)[1] LDN 0088050 significantly inhibits LPS-induced expression of both TNFα and IL-6 in RAW264.7 cells[1]. [1]. Zhou Y, et al. The discovery of novel and selective fatty acid binding protein 4 inhibitors by virtual screening and biolo...

化合物

Cat.No: T15622

Synonym: JNJ-5446

Target: P2X Receptor

Cat.No: T36347

Synonym: Caspase-1 Inhibitor II,Ac-Tyr-Val-Ala-Asp-chloromethylketone,Ac-Tyr-Val-Ala-Asp-CMK

Target: IL Receptor, Caspase, Immunology/Inflammation related, Pyroptosis

Cat.No: T6090

Synonym: VX-765

Target: Caspase

Lyn peptide inhibitor acetate

Cat.No: TP2008L

Synonym: Lyn peptide inhibitor acetate(222018-18-0 free base)

Target: IL Receptor

Cat.No: T16570

Synonym: VX-740,HMR 3480

Target: Others

Cat.No: T70905

NLRP3 agonist 1

Cat.No: T81668

Target: NOD-like Receptor (NLR)

Cat.No: T76938

Cat.No: T10447

Target: Others

Cat.No: T78822

Target: NOD-like Receptor (NLR)

Cat.No: T61621

Cat.No: T68225

P2X7 receptor antagonist-4

Cat.No: T81579

C18 Phytoceramide (t18:0/18:0)

Cat.No: T37458

Cat.No: T74908

C6 L-threo Ceramide (d18:1/6:0)

Cat.No: T36320

Synonym: C6 L-threo Ceramide (d18:1/6:0)

C6 D-threo Ceramide (d18:1/6:0)

Cat.No: T37565

Synonym: C6 D-threo Ceramide (d18:1/6:0)

Cat.No: T69815

Cat.No: T36629

Cat.No: T37614

Cat. No.	Product Name	Target	Signaling Pathways
T9352	hydrocotarnine	Others	Others
	hydrocotarnine 是 Cbl 的抑制剂。
T37280	PE(18:1(9Z)/0:0)	Endogenous Metabolite	Metabolism
	PE(18:1(9Z)/0:0) 是一种天然存在的溶血磷脂，是缩醛磷脂溶血磷脂酰乙醇胺的类似物。 PE(18:1(9Z)/0:0) 以浓度依赖性方式诱导 PC12 大鼠神经元细胞中细胞内钙的瞬时增加。 PE(18:1(9Z)/0:0) 增加 IL-4 和 IL-2 的产生，但不增加 IFN-γ 的产生。在小鼠血清中，PE(18:1(9Z)/0:0)（1 μg/动物）诱导 T 辅助细胞 2 反应。在寒冷暴露三天后，小鼠肩胛间棕色脂肪组织中的 PE(18:1(9Z)/0:0) 水平增加。
T7009	Soyacerebroside II	IL Receptor; Calcium Channel	Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism
	Soyacerebroside II exhibits ionophoretic activity for Ca2+ ion. Soyacerebrosides I and II have modulating the cellular immune response effects, they show obvious inhibitory activity on IL-18 secretion in human peripheral blood mononuclear cells (PBMC).
T38838	QS-21 Stimulon,QS-21
	QS-21, an immunostimulatory saponin, is a powerful vaccine adjuvant that stimulates both Th2 humoral and Th1 cell-mediated immune responses by interacting with antigen presenting cells (APCs) and T cells. Additionally, QS-21 activates the NLRP3 inflammasome, leading to the release of cytokines IL-1β and IL-18, which are dependent on caspase-1.

天然产物

Cat.No: T9352

Target: Others

PE(18:1(9Z)/0:0)

Cat.No: T37280

Target: Endogenous Metabolite

Soyacerebroside II

Cat.No: T7009

Target: IL Receptor, Calcium Channel

Cat.No: T38838

Synonym: Stimulon,QS-21

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